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SR 144528
- Soluble in DMSO
- MF: C29H34ClN3O
- MW: 476.05
Description
SR 144528 is a potent and highly selective cannabinoid CB2 receptor antagonist/inverse agonist with a reported Ki value of 0.6 nM at CB2.
CB2 receptors are enriched in immune cells and regulate inflammatory, nociceptive and immunomodulatory cannabinoid signaling. SR 144528 is useful for CB2 receptor pharmacology with reported selectivity over CB1 receptors.
Key Features
- Potent CB2 antagonist/inverse agonist
- Ki: 0.6 nM at CB2
- Approximately 400 nM affinity at CB1 in reported assays
- Useful probe for immune-related cannabinoid signaling
Applications
- CB2 receptor binding and functional assays
- Cannabinoid receptor selectivity studies
- Inflammation and immune-cell signaling research
- Inverse agonist pharmacology profiling
More Information
| Parent CAS No. | 192703-06-3 |
|---|---|
| Chemical Name | 5-(4-chloro-3-methylphenyl)-1-(4-methylbenzyl)-N-((1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]heptan-2-yl)-1H-pyrazole-3-carboxamide |
| MFCD | MFCD05662316 |
| Short Description | CB2 antagonist |
References
- M Rinaldi-Carmona et al. SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. J. Pharmacol. Exp. Ther. 1998, 284 (2), 644–50.
- M Portier et al. SR 144528, an antagonist for the peripheral cannabinoid receptor that behaves as an inverse agonist. J. Pharmacol. Exp. Ther. 1999, 288 (2), 582-589.
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